Synthesis and evaluation of 8-deaza-5,6,7,8-tetrahydromethotrexate derivatives as dihydrofolate reductase inhibitors

doi:10.5246/jcps.2012.02.018

Abstract

Abstract:

A series of N⁵-substituted 8-deaza-5,6,7,8-tetrahydromethotrexate derivatives were synthesized and evaluated as inhibitors of dihydrofolate reductase (DHFR). The results indicated that modification of the pteridine ring of methotrexate (MTX) rendered poor activity against human DHFR.

Key words: 8-Deaza-5,6,7,8-tetrahydromethotrexate, Synthesis, Dihydrofolate reductase inhibitory activities

CLC Number:

R916.41

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Chao Tian, Zhi-Li Zhang, Jun-Yi Liu^*

. Synthesis and evaluation of 8-deaza-5,6,7,8-tetrahydromethotrexate
derivatives as dihydrofolate reductase inhibitors [J]. , DOI: 10.5246/jcps.2012.02.018.

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URL: http://jcps.bjmu.edu.cn/EN/10.5246/jcps.2012.02.018

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